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Chem Biol. 2010 Nov 24;17(11):1171-6. doi: 10.1016/j.chembiol.2010.09.008.

Assembling ligands in situ using bioorthogonal boronate ester synthesis.

Author information

1
Department of Pharmacology, Weill Medical College, Cornell University, New York, NY 10065, USA.

Abstract

Many molecules that could manipulate cellular function are not practical due to their large size and concomitant undesirable pharmocokinetic properties. Here, we describe a bioorthogonal, highly stable boronate ester (HiSBE) synthesis and use this reaction to synthesize a biologically active molecule from smaller precursors in a physiological context. The rapid rate of HiSBE synthesis suggests that it may be useful for assembling a wide variety of biologically active molecules in physiological solutions.

PMID:
21095566
PMCID:
PMC3149976
DOI:
10.1016/j.chembiol.2010.09.008
[Indexed for MEDLINE]
Free PMC Article

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